α-Bisabolol is a naturally occurring sesquiterpene alcohol which was first isolated from Matricaria chamomilla (Asteraceae) in the 20th century and has since been identified in other aromatic plants such as Eremanthus erythropappus, Smyrniopsis aucheri and Vanillosmopsis species. Recently, α-bisabolol was identified as a major constituent of Salvia runcinata essential oil, a plant indigenous to South Africa. The use of α-bisabolol or bisabolol-rich oil as an anti-inflammatory agent is ubiquitous. This compound also exhibits several other pharmacological properties such as analgesic, antibiotic and anticancer activities. Mutagenicity and genotoxicity of bisabolol have also been investigated. Due to the low toxicity associated with bisabolol the Food and Drug Administration (FDA) has granted this constituent with GRAS status (Generally Regarded as Safe) which has promoted its use as an active ingredient in several commercial products. This review aims to summarise the role of α-bisabolol in pharmacological and/or physiological processes and to discuss some of the possible mechanisms of action of this commercially important molecule.